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Synthesis, bioactivity evaluation and computational studies of bisindolylmethane and flavone derivatives / Syahrul Imran Abu Bakar

Bisindolylmethane and flavone are well-known natural product scaffolds having important pharmacophores and they have gained tremendous interest owing to their remarkable potency and activity profile towards various target diseases. In this study novel bisindolylmethanes and flavones were synthesized...

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Main Author: Abu Bakar, Syahrul Imran
Format: Book Section
Language:English
Published: Institute of Graduate Studies, UiTM 2016
Subjects:
Malaysia
Online Access:http://ir.uitm.edu.my/id/eprint/20120/1/ABS_SYAHRUL%20IMRAN%20ABU%20BAKAR%20TDRA%20VOL%2010%20IGS%2016.pdf
http://ir.uitm.edu.my/id/eprint/20120/
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spelling my.uitm.ir.201202018-06-11T04:14:37Z http://ir.uitm.edu.my/id/eprint/20120/ Synthesis, bioactivity evaluation and computational studies of bisindolylmethane and flavone derivatives / Syahrul Imran Abu Bakar Abu Bakar, Syahrul Imran Malaysia Bisindolylmethane and flavone are well-known natural product scaffolds having important pharmacophores and they have gained tremendous interest owing to their remarkable potency and activity profile towards various target diseases. In this study novel bisindolylmethanes and flavones were synthesized to identify potential inhibitors for bacterial infection, cancer, and diabetes. One hundred twenty-nine (129) bisindolylmethane derivatives (Schiff base, thiourea, sulfonamide, and hydrazone) and 43 flavone derivatives (hydrazone and ether) were synthesized, evaluated for various in vitro bioactivities, and analyzed through computational studies to identify possible inhibition mechanisms. Antibacterial activity of bisindolylmethane Schiff bases showed that most compounds moderately inhibit Salmonella typhi, S. paratyphi A and S. paratyphi B bacterial strains. The results also reveals that compounds having halides and nitro substituents showed best antibacterial activity. Bisindolylmethane thioureas and sulfonamides were tested for carbonic anhydrase II inhibition activity. Molecular docking results suggest that nitro substituent at para position interacts well with Zn2+ ion and interferes with the Zn-OH-Thr199-Glu106 hydrogen bond network. Bisindole hydrazone in this study were synthesized through a three-step reaction. β-Glucuronidase inhibitory property of some derivatives were found to be very potent (0.1-83.5 μM). Docking studies showed that active compounds should have two or more hydroxyl groups substituted on carbon adjacent to each other for good interactions to take place… Institute of Graduate Studies, UiTM 2016 Book Section PeerReviewed text en http://ir.uitm.edu.my/id/eprint/20120/1/ABS_SYAHRUL%20IMRAN%20ABU%20BAKAR%20TDRA%20VOL%2010%20IGS%2016.pdf Abu Bakar, Syahrul Imran (2016) Synthesis, bioactivity evaluation and computational studies of bisindolylmethane and flavone derivatives / Syahrul Imran Abu Bakar. In: The Doctoral Research Abstracts. IGS Biannual Publication, 10 (10). Institute of Graduate Studies, UiTM, Shah Alam.
institution Universiti Teknologi Mara
building Tun Abdul Razak Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Teknologi Mara
content_source UiTM Institutional Repository
url_provider http://ir.uitm.edu.my/
language English
topic Malaysia
spellingShingle Malaysia
Abu Bakar, Syahrul Imran
Synthesis, bioactivity evaluation and computational studies of bisindolylmethane and flavone derivatives / Syahrul Imran Abu Bakar
description Bisindolylmethane and flavone are well-known natural product scaffolds having important pharmacophores and they have gained tremendous interest owing to their remarkable potency and activity profile towards various target diseases. In this study novel bisindolylmethanes and flavones were synthesized to identify potential inhibitors for bacterial infection, cancer, and diabetes. One hundred twenty-nine (129) bisindolylmethane derivatives (Schiff base, thiourea, sulfonamide, and hydrazone) and 43 flavone derivatives (hydrazone and ether) were synthesized, evaluated for various in vitro bioactivities, and analyzed through computational studies to identify possible inhibition mechanisms. Antibacterial activity of bisindolylmethane Schiff bases showed that most compounds moderately inhibit Salmonella typhi, S. paratyphi A and S. paratyphi B bacterial strains. The results also reveals that compounds having halides and nitro substituents showed best antibacterial activity. Bisindolylmethane thioureas and sulfonamides were tested for carbonic anhydrase II inhibition activity. Molecular docking results suggest that nitro substituent at para position interacts well with Zn2+ ion and interferes with the Zn-OH-Thr199-Glu106 hydrogen bond network. Bisindole hydrazone in this study were synthesized through a three-step reaction. β-Glucuronidase inhibitory property of some derivatives were found to be very potent (0.1-83.5 μM). Docking studies showed that active compounds should have two or more hydroxyl groups substituted on carbon adjacent to each other for good interactions to take place…
format Book Section
author Abu Bakar, Syahrul Imran
author_facet Abu Bakar, Syahrul Imran
author_sort Abu Bakar, Syahrul Imran
title Synthesis, bioactivity evaluation and computational studies of bisindolylmethane and flavone derivatives / Syahrul Imran Abu Bakar
title_short Synthesis, bioactivity evaluation and computational studies of bisindolylmethane and flavone derivatives / Syahrul Imran Abu Bakar
title_full Synthesis, bioactivity evaluation and computational studies of bisindolylmethane and flavone derivatives / Syahrul Imran Abu Bakar
title_fullStr Synthesis, bioactivity evaluation and computational studies of bisindolylmethane and flavone derivatives / Syahrul Imran Abu Bakar
title_full_unstemmed Synthesis, bioactivity evaluation and computational studies of bisindolylmethane and flavone derivatives / Syahrul Imran Abu Bakar
title_sort synthesis, bioactivity evaluation and computational studies of bisindolylmethane and flavone derivatives / syahrul imran abu bakar
publisher Institute of Graduate Studies, UiTM
publishDate 2016
url http://ir.uitm.edu.my/id/eprint/20120/1/ABS_SYAHRUL%20IMRAN%20ABU%20BAKAR%20TDRA%20VOL%2010%20IGS%2016.pdf
http://ir.uitm.edu.my/id/eprint/20120/
_version_ 1685649304424808448
score 13.211869

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